申请人:Endocyte, Inc.
公开号:US20160220694A1
公开(公告)日:2016-08-04
The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.
该发明描述了一种维生素受体结合药物传递共轭物及其制备方法。药物传递共轭物由维生素受体结合基团、双价连接剂(L)和药物组成。维生素受体结合基团包括维生素、维生素受体结合类似物及其衍生物,药物包括类似物及其衍生物。维生素受体结合基团与双价连接剂共价连接,药物或其类似物或衍生物与双价连接剂共价连接,其中双价连接剂(L)包括间隔连接剂、可释放连接剂和杂原子连接剂以及其组合。还描述了利用该药物传递共轭物消除病原细胞群的方法和药物组合物。